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Difamilast

Catalog No. T27172 CAS 937782-05-3

Difamilast is a selective inhibitor of phosphodiesterase-4 (PDE4) with particularly efficient inhibition of subtype B (IC50=11.2 nM).

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Difamilast, CAS 937782-05-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 132.00
5 mg	In stock	$ 328.00
10 mg	In stock	$ 528.00
25 mg	In stock	$ 859.00
50 mg	In stock	$ 1,190.00
100 mg	In stock	$ 1,580.00
1 mL * 10 mM (in DMSO)	In stock	$ 363.00

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Purity: 99.04%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Difamilast is a selective inhibitor of phosphodiesterase-4 (PDE4) with particularly efficient inhibition of subtype B (IC50=11.2 nM).
Targets&IC50	PDE4B:11.2 nM
In vitro	Difamilast exerts inhibitory effects on PDE2[1].
In vivo	In relevant animal models of AD, Difamilast improves skin condition [3].

Molecular Weight	446.44
Formula	C23H24F2N2O5
CAS No.	937782-05-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (223.99 mM)

References and Literature

1. Ahluwalia J, et, al. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook. Drugs. 2017 Sep;77(13):1389-1397. 2. Soeberdt M, et, al. Small molecule drugs for the treatment of pruritus in patients with atopic dermatitis. Eur J Pharmacol. 2020 Aug 15;881:173242. 3. Hanifin JM, et, al. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-controlled study. J Am Acad Dermatol. 2016 Aug;75(2):297-305.

Citations

1. Mikheil D, Larsen M A, Hsiao K, et al.A bioluminescent and homogeneous assay for monitoring GPCR-mediated cAMP modulation and PDE activity.Scientific Reports.2024, 14(1): 4440.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compounds Library Max Metabolism Compound Library Approved Drug Library Bioactive Compound Library Pediatric Drug Library

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CP671305 ONO-8430506 GSK356278 PDE7-IN-2 Zatolmilast Apremilast-d5 PQ-10 Luteolin

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Difamilast 937782-05-3 Metabolism PDE PDE4 OPA 15406 Inhibitor atopic phosphodiesterase-4 OPA15406 Phosphodiesterase (PDE) OPA-15406 dermatitis subtype inhibit inhibitor

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